CL2016002072A1 - 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer - Google Patents

2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer

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Publication number
CL2016002072A1
CL2016002072A1 CL2016002072A CL2016002072A CL2016002072A1 CL 2016002072 A1 CL2016002072 A1 CL 2016002072A1 CL 2016002072 A CL2016002072 A CL 2016002072A CL 2016002072 A CL2016002072 A CL 2016002072A CL 2016002072 A1 CL2016002072 A1 CL 2016002072A1
Authority
CL
Chile
Prior art keywords
trifluoro
alzheimer
disease
amino
treatment
Prior art date
Application number
CL2016002072A
Other languages
English (en)
Spanish (es)
Inventor
Karsten Juhl
Mauro Marigo
Lena Tagmose
Thomas Jensen
Original Assignee
H Lundbeck As
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by H Lundbeck As filed Critical H Lundbeck As
Publication of CL2016002072A1 publication Critical patent/CL2016002072A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D227/00Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
    • C07D227/02Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D227/06Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D227/10Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
CL2016002072A 2014-02-19 2016-08-17 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer CL2016002072A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA201400086 2014-02-19
DKPA201400349 2014-07-01

Publications (1)

Publication Number Publication Date
CL2016002072A1 true CL2016002072A1 (es) 2017-01-20

Family

ID=59009438

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2016002072A CL2016002072A1 (es) 2014-02-19 2016-08-17 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer

Country Status (25)

Country Link
US (2) US20170066741A1 (hr)
EP (1) EP3107897A1 (hr)
JP (1) JP6483146B2 (hr)
KR (1) KR20160115936A (hr)
CN (1) CN106029639B (hr)
AP (1) AP2016009370A0 (hr)
AR (1) AR099489A1 (hr)
AU (1) AU2015220873A1 (hr)
CA (1) CA2940028A1 (hr)
CL (1) CL2016002072A1 (hr)
CR (1) CR20160352A (hr)
DO (1) DOP2016000194A (hr)
EA (1) EA031132B1 (hr)
EC (1) ECSP16072941A (hr)
GE (1) GEP20186892B (hr)
IL (1) IL246875A0 (hr)
MA (1) MA39225A1 (hr)
MX (1) MX2016010777A (hr)
PE (1) PE20161225A1 (hr)
PH (1) PH12016501600A1 (hr)
RU (1) RU2016133626A (hr)
SG (1) SG11201606812WA (hr)
TW (1) TW201609700A (hr)
UA (1) UA117695C2 (hr)
WO (1) WO2015124576A1 (hr)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
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WO2015124576A1 (en) 2014-02-19 2015-08-27 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
JO3627B1 (ar) 2015-04-30 2020-08-27 H Lundbeck As إيميدازو بيرازينونات على هيئة مثبطات pde1
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
TW201718543A (zh) 2015-08-12 2017-06-01 H 朗德貝克公司 作爲bace1抑制劑之2-胺基-3-氟-3-(氟甲基)-6-甲基-6-苯基-3,4,5,6-四氫吡啶
EP3347486A4 (en) 2015-09-09 2019-06-19 The Trustees of Columbia University in the City of New York REDUCTION OF ER-MAM-LOCALIZED APP-C99 AND METHOD FOR THE TREATMENT OF ALZHEIMER DISEASE
TW201726651A (zh) * 2015-09-23 2017-08-01 健生藥品公司 2,3,4,5-四氫吡啶-6-胺衍生物
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
WO2018078038A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders
JP2020500841A (ja) 2016-10-28 2020-01-16 ハー・ルンドベック・アクチエゼルスカベット イミダゾピラジノンの投与を含む併用療法
WO2018114910A1 (en) 2016-12-21 2018-06-28 H. Lundbeck A/S 6-amino-5-fluoro-5-(fluoromethyl)-2,3,4,5-tetrahydropyridin-2-yl-phenyl-5-(methoxy-d3)-pyrazine-2-carboxamides and fluorinated derivatives thereof as bace1 inhibitors
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
US11634416B2 (en) 2017-12-14 2023-04-25 H. Lundbeck A/S Combination treatments comprising administration of 1H-pyrazolo[4,3-b]pyridines
CN111511742B (zh) 2017-12-20 2023-10-27 H.隆德贝克有限公司 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶
KR102507861B1 (ko) 2018-04-19 2023-03-09 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법
KR102510077B1 (ko) 2018-04-24 2023-03-14 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법

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TW201623295A (zh) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 具有bace1抑制活性之二氫噻及二氫衍生物

Also Published As

Publication number Publication date
CA2940028A1 (en) 2015-08-27
JP2017506237A (ja) 2017-03-02
CN106029639A (zh) 2016-10-12
SG11201606812WA (en) 2016-09-29
MX2016010777A (es) 2016-10-26
DOP2016000194A (es) 2016-09-30
CN106029639B (zh) 2019-01-08
CR20160352A (es) 2016-10-20
EA201691447A1 (ru) 2016-12-30
ECSP16072941A (es) 2017-02-24
US9353084B2 (en) 2016-05-31
WO2015124576A1 (en) 2015-08-27
JP6483146B2 (ja) 2019-03-13
GEP20186892B (en) 2018-09-10
AU2015220873A1 (en) 2016-08-11
UA117695C2 (uk) 2018-09-10
EP3107897A1 (en) 2016-12-28
AP2016009370A0 (en) 2016-08-31
TW201609700A (zh) 2016-03-16
EA031132B1 (ru) 2018-11-30
PH12016501600A1 (en) 2017-02-06
RU2016133626A (ru) 2018-03-20
IL246875A0 (en) 2016-08-31
US20150232449A1 (en) 2015-08-20
MA39225A1 (fr) 2017-04-28
PE20161225A1 (es) 2016-12-04
RU2016133626A3 (hr) 2018-09-25
AR099489A1 (es) 2016-07-27
US20170066741A1 (en) 2017-03-09
KR20160115936A (ko) 2016-10-06

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